Russo G L, Della Pietra V, Mercurio C, Della Ragione F, Marshak D R, Oliva A, Zappia V
I.S.A. Institute of Food Science and Technology, National Research Council, Avellino, Italy.
Biochem Biophys Res Commun. 1997 Apr 28;233(3):673-7. doi: 10.1006/bbrc.1997.6515.
Butyrate, a dietary fiber derivative, is a well-known differentiating agent in cultured cell lines. In addition, its antineoplastic activity toward colon-rectum cancers has been documented both in vivo and in vitro. Despite the large amount of information on the potential clinical efficacy of butyrate, its mechanism of action at the molecular level has only been partially investigated. Here, we show that serine/threonine protein kinase CKII is a target of butyrate activity. In the human adenocarcinoma cell line, HT29, treated with 2 mM sodium butyrate, CKII activity decreases 50% at 24 and 48 hours after drug addition. The enzyme down-regulation is not due to changes in protein amount since the levels of the different CKII subunits remain constant during butyrate treatment. The data reported provide the first evidence that CKII down-regulation is involved in the signal transduction pathway started by butyrate.
丁酸盐是一种膳食纤维衍生物，是培养细胞系中著名的分化剂。此外，其对结直肠癌的抗肿瘤活性已在体内和体外得到证实。尽管有大量关于丁酸盐潜在临床疗效的信息，但其分子水平的作用机制仅得到部分研究。在此，我们表明丝氨酸/苏氨酸蛋白激酶CKII是丁酸盐活性的靶点。在人腺癌细胞系HT29中，用2 mM丁酸钠处理后，添加药物24小时和48小时后CKII活性降低50%。酶的下调并非由于蛋白量的变化，因为在丁酸盐处理期间不同CKII亚基的水平保持恒定。所报道的数据首次证明CKII下调参与了由丁酸盐启动的信号转导途径。
